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Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System

Abdelmonem, Rehab ; Azer, Marian Sobhy ; Makky, Amna ; Zaghloul, Abdelazim ; El-Nabarawi, Mohamed ; Nada, Aly

Drug design, development and therapy, 2020-01, Vol.14, p.4343-4362 [Periódico revisado por pares]

New Zealand: Dove Medical Press Limited

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Título:
Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System
Autor: Abdelmonem, Rehab ; Azer, Marian Sobhy ; Makky, Amna ; Zaghloul, Abdelazim ; El-Nabarawi, Mohamed ; Nada, Aly
Assuntos: Adsorption ; aeroperl® 300 ; Animals ; Anticonvulsants - administration & dosage ; Anticonvulsants - pharmacokinetics ; antiepileptic drug ; Bioavailability ; Biological Availability ; Calorimetry ; Calorimetry, Differential Scanning ; Convulsions & seizures ; Crystallography, X-Ray ; Design of experiments ; Differential scanning calorimetry ; Diffraction ; Dilution ; Dissolution ; Drug Carriers ; Drug Compounding ; Drug delivery ; Drug Delivery Systems ; Drug Design ; Drug dosages ; Drug Stability ; Drugs ; Electric equipment industry ; Electrical equipment and supplies industry ; Emulsification ; Emulsions ; Factorial design ; Instrument industry ; Instrument industry (Equipment) ; Ischemia ; Lamotrigine ; Lamotrigine - administration & dosage ; Lamotrigine - pharmacokinetics ; lipid-based formulation ; Microemulsions ; Nanoemulsions ; Optimization ; oral bioavailability ; Original Research ; Particle size ; Pharmaceutical industry ; Pharmacokinetics ; Phosphates ; Polyethylene glycol ; porous carriers ; Rabbits ; Ratios ; Scanning electron microscopy ; Software ; Solids ; Solubility ; Surface active agents ; Surfactants ; Tablets ; Thermodynamics ; Vehicles ; X ray powder diffraction ; X-ray diffraction ; X-rays
É parte de: Drug design, development and therapy, 2020-01, Vol.14, p.4343-4362
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Descrição: This study aimed to prepare solid self-nanoemulsified drug delivery system (S-SNEDDS) of lamotrigine (LMG) for enhancing its dissolution and oral bioavailability (BA). Nineteen liquid SNEDDS were prepared (R1-R19) using D-optimal design with different ratios of oil, surfactant (S), and cosurfactant (Cos). The formulations were characterized regarding robustness to dilution, droplet size, thermodynamic stability testing, self-emulsification time, in-vitro release in 0.1 N HCl and phosphate buffer (PB; pH 6.8). Design Expert 11 software was used to select the optimum formulations. Eight S-SNEDDS were prepared (S1-S8) using 2 factorial design, and characterized by differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), and scanning electron microscopy (SEM). The optimum formulation was chosen regarding in-vitro drug released in 0.1 N HCl and PB, compared to pure LMG and commercial tablet (Lamictal ). The BA of LMG from the optimized S-SNEDDS formulation was evaluated in rabbits compared to pure LMG and Lamictal . The optimized S-SNEDDS was S2, consisting of R9 adsorbed on Aeroperl 300 in a ratio of 1:1, with the best results regarding in-vitro drug released in 0.1 N HCl at 15 min (100%) compared to pure LMG (73.40%) and Lamictal (79.43%), and in-vitro drug released in PB at 45 min (100%) compared to pure LMG (30.46%) and Lamictal (92.08%). DSC, PXRD, and SEM indicated that LMG was molecularly dispersed within the solid nano-system. The BA of S2 was increased 2.03 and 1.605 folds compared to pure LMG, and Lamictal , respectively. S2 is a promising S-SNEDDS formulation. It can be a potential carrier for improving dissolution, and BA of LMG.
Editor: New Zealand: Dove Medical Press Limited
Idioma: Inglês

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Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System

Abdelmonem, Rehab ; Azer, Marian Sobhy ; Makky, Amna ; Zaghloul, Abdelazim ; El-Nabarawi, Mohamed ; Nada, Aly

New Zealand: Dove Medical Press Limited

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